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The Use of GPCR Structures in Drug Design
II. Technology Developments Enabling GPCR Structure Determination
III. GPCR Structures
IV. GPCR Structures in Drug Discovery
Allosteric Modulation of Metabotropic Glutamate Receptors
II. Metabotropic Glutamate Receptors
III. Pharmacological Profiles of mGlu Allosteric Modulators
IV. Quantifying Allosteric Interactions
V. Structural Determinants of mGlu Allosteric Modulator Binding
VI. Functional Selectivity of mGlu Allosteric Modulation
VII. Therapeutic Potential of mGlu Allosteric Modulators
II. GPCRs as Conformational Ensembles
III. The Pluridimensional Nature of GPCR Efficacy
IV. Functionally Selective GPCR Agonism
V. Functional Selectivity and Pharmaceutical Development
VI. Functional Selectivity at the Parathyroid Hormone Receptor
Pharmacological Chaperones for Misfolded Gonadotropin-Releasing Hormone Receptors
II. The Endoplasmic Reticulum Quality Control System
III. Misfolding of GPCRs and Disease
IV. Mutations in the Human GnRHR
V. Rescue of Misfolded hGnRHR Mutants with Pharmacoperones
VI. Mechanism of Action of Pharmacoperones
VII. The Dominant-Negative Effect of hGnRHR Mutants and Receptor Rescue
Regulation of Stability and Trafficking of Calcium-Sensing Receptors by Pharmacologic Chaperones
II. CaSR: Physiological Contributions to Calcium Homeostasis
III. CaSR and Disease
IV. Posttranslational Mechanisms Controlling CaSR Abundance
V. Pharmacologic Chaperone Contributions to Plasma Membrane Targeting of CaSR
VI. Pharmacologic Chaperone Regulation of Organellar CaSR
Experimental Challenges to Targeting Poorly Characterized GPCRs
II. Deorphanization of the Receptors for FFAs
III. Uncovering the Pharmacology of FFA Receptors
IV. Synthetic Ligands for FFA Receptors
V. Therapeutic Potential for FFA Receptors
Biological and Pharmacological Roles of HCA Receptors
II. Identification and Characterization of HCA Receptors
III. Gene Structure and Tissue Distribution
IV. Physiological and Pharmacological Roles of HCA Receptors
V. Receptor Classification with Pharmacological Tools
VI. Mutagenesis and Receptor-Modeling Studies
VII. Signal Transduction and Receptor Desensitization
VIII. Therapeutic Potential of HCA Receptor Ligands
Pharmacology, Signaling and Physiological Relevance of the G Protein-coupled Receptor 55
II. The G Protein-Coupled Receptor 55
III. Biological Relevance of GPR55
Role of PDZ Proteins in Regulating Trafficking, Signaling, and Function of GPCRs
II. PDZ Proteins
III. GPCRs with Carboxy-Terminal PDZ Recognition Motifs
IV. PDZ Protein Regulation of GPCR Signaling
Regulator of G Protein Signaling Proteins as Drug Targets
II. RGS Proteins Regulate Signaling via GPCRs
III. Regulation of RGS Protein Function and Expression
IV. Noncanonical Functions of RGS Proteins
V. Biological Functions of RGS Proteins—Implications in Drug Discovery
VI. Advances in RGS Protein Drug Discovery
VII. The Future of Targeting RGS Proteins in Drug Discovery
GPCR-Interacting Proteins, Major Players of GPCR Function
II. Biosynthesis and Cell Surface Targeting of GPCRs
III. Modulation of GPCR Signaling
IV. Endocytosis and Recycling of GPCRs
G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists.
- The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors
- It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones
- This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists
Pharmacologists, immunologists, and biochemists
- No. of pages:
- © Academic Press 2011
- 19th September 2011
- Academic Press
- Hardcover ISBN:
- eBook ISBN:
Dr. S. J. Enna received his B.A. degree (1965, Biology) from Rockhurst University, Kansas City, Missouri and both his M.S. (1967, Pharmacology) and Ph.D. (1970, Pharmacology) degrees from the University of Missouri-Kansas City. Postdoctoral training in pharmacology was completed at the University of Texas Southwestern Medical School in Dallas, at F. Hoffmann La Roche in Basel, Switzerland, and the Department of Pharmacology and Experimental Therapeutics at Johns Hopkins University School of Medicine in Baltimore. Dr. Enna spent 10 years on the faculty at the University of Texas Medical School at Houston in the Departments of Pharmacology and Neurobiology. While at the University of Texas Dr. Enna was also a consultant for ICI USA, Inc., Merck, Sharp and Dohme Research Laboratories, Bristol Myers Corporation, and Panlabs, Inc. From 1986 1990, Dr. Enna was Senior Vice President and Scientific Director of Nova Pharmaceutical Corporation in Baltimore, and Executive Vice President from 1990 1992. He is currently Associate Dean for Research and Graduate Education as well as Professor of Physiology and of Pharmacology at the University of Kansas Medical School. Dr. Enna served as chair of the Department of Pharmacology, Toxicology and Therapeutics at the University of Kansas Medical School from 1992 to 2003. Other previous academic appointments include Lecturer in the Department of Neuroscience at The Johns Hopkins University School of Medicine in Baltimore and Adjunct Professor of Pharmacology at Tulane University School of Medicine in New Orleans.
Dr. Enna served for six years as editor of The Journal of Pharmacology and Experimental Therapeutics, and is currently co-editor of Current Protocols in Pharmacology. He is also Editor-in-Chief of Biochemical Pharmacology, Executive Editor-in-Chief of Pharmacology and Therapeutics and Series Editor of Advances in Pharmacology. Besides his editorships, Dr. Enna serves on the editorial boards of Brain Research, Life Sciences and CNS Drug Reviews. He has been the recipient of Research Career Development Awards from the National Institute of Mental Health and the National Institute for Neurological, Communicative Disorders and Stoke. Other awards include the John Jacob Abel Award and the Torald Sollmann Award from the American Society for Pharmacology and Experimental Therapeutics, the Daniel H. Efron Award from the American College of Neuropsychopharmacology, and a PhARMA Foundation Excellence Award. In recent years he has been a member of the Scientific Advisory Council of Abbott Laboratories, has served on the Board of Directors of the Life Sciences Research Office, and on the Scientific Advisory Board of the National Alliance for Autism Research. He is currently a member of the Basic Pharmacology Advisory Committee of the PhARMA Foundation. Dr. Enna has held many elective offices in professional societies including the presidency of the American Society for Pharmacology and Experimental Therapeutics (ASPET). Since 2006 he has served as Secretary General of the International Union of Basic and Clinical Pharmacology (IUPHAR).
Dr. Enna's research interests include neuropharmacology, neurochemistry and neuropsychiatric disorders. He has made significant contributions in defining the pharmacological and biochemical properties of neurotransmitter receptors, in particular those for GABA. He has also conducted research into the effects of hormones on neurotransmitter receptor function and receptor responses to psychotherapeutics, the development of receptor antagonists for NMDA, cholinergic muscarinic and bradykinin receptors, and the identification of the cellular components of coincident signaling in brain. Dr. Enna's research is described in over 200 published research reports, reviews, and book chapters. He has authored or edited over three dozen books on topics ranging from neuropharmacology in general, to neurotransmitter receptors and GABA.
Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, USA
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